RGD-peptide conjugated inulin-ibuprofen nanoparticles for targeted delivery of Epirubicin.
RGD-peptide conjugated inulin-ibuprofen nanoparticles for targeted delivery of Epirubicin.
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DOI：
10.1016/j.colsurfb.2016.03.077
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发表时间：
2016-08
期刊：
影响因子：
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通讯作者：
Luzhong Zhang;Guicai Li;Ming Gao;Xin Liu;B. Ji;Ruheng Hua;Y. Zhou;Yumin Yang
中科院分区：
文献类型：
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作者：
Luzhong Zhang;Guicai Li;Ming Gao;Xin Liu;B. Ji;Ruheng Hua;Y. Zhou;Yumin Yang
近年来，基于化疗的聚合物纳米颗粒在实体瘤治疗中得到了广泛的研究。肿瘤靶向纳米颗粒显示出改善肿瘤组织积累的巨大潜力，优越的抗癌活性和减少副作用。因此，通过菊粉与布洛芬之间的酯化反应合成了菊粉-布洛芬聚合物，并通过菊粉-布洛芬聚合物的自组装和EPB的原位包封制备了RGD靶向表阿霉素（EPB）纳米颗粒。采用动态光散射（DLS）和透射电子显微镜（TEM）对RGD共轭EPB负载纳米粒子进行了表征。EPB的释放呈pH依赖性，并随着pH值的降低而加速，有利于药物在体内的有效释放。细胞内摄取分析表明，RGD结合的纳米颗粒很容易被癌细胞内化。体外细胞毒性实验表明，RGD结合的EPB纳米颗粒比未结合的EPB纳米颗粒具有更好的抗肿瘤效果。更重要的是，通过体内抗肿瘤活性、EPB的生物分布和组织学分析，RGD共轭EPB负载纳米粒子比游离EPB和非共轭EPB纳米粒子具有更好的抗癌效果和更低的毒性。
Recently, chemotherapy-based polymeric nanoparticles have been extensively investigated for solid tumor treatment. Tumor targeted nanoparticles demonstrated great potential for improved accumulation in the tumor tissue, superior anticancer activity and reduced side effects. Thus, inulin-ibuprofen polymer was synthesized by esterification between inulin and ibuprofen, and RGD targeted epirubicin (EPB) loaded nanoparticles were prepared by the self-assembly of inulin-ibuprofen polymer and in situ encapsulation of EPB. RGD conjugated EPB loaded nanoparticles were characterized by dynamic light scattering (DLS) and transmission electron microscope (TEM). The EPB release from the nanoparticles showed pH-dependent profile and accelerated by the decreased pH value, which would favor the effective drug deliveryin vivo. Intracellular uptake analysis suggested that RGD conjugated nanoparticles could be easily internalized by the cancer cells.In vitrocytotoxicity revealed that RGD conjugated EPB loaded nanoparticles exhibited the better antitumor efficacy compared with non-conjugated nanoparticles. More importantly, RGD conjugated EPB loaded nanoparticles showed superior anticancer effects and reduced toxicity than free EPB and non-conjugated nanoparticles byin vivoantitumor activity, EPB biodistribution and histology analysis.